WO2011003858A3 - Pharmaceutical compositions and solid forms - Google Patents

Pharmaceutical compositions and solid forms Download PDF

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Publication number
WO2011003858A3
WO2011003858A3 PCT/EP2010/059553 EP2010059553W WO2011003858A3 WO 2011003858 A3 WO2011003858 A3 WO 2011003858A3 EP 2010059553 W EP2010059553 W EP 2010059553W WO 2011003858 A3 WO2011003858 A3 WO 2011003858A3
Authority
WO
WIPO (PCT)
Prior art keywords
yloxy
pyrimidin
hydroxymethyl
amide
phenyl
Prior art date
Application number
PCT/EP2010/059553
Other languages
French (fr)
Other versions
WO2011003858A2 (en
Inventor
Joerg Berghausen
Claire Haug
Michael Herbig
Bin Hu
Stéphane JONAT
Rajender Leleti
Josef Gottfried Meingassner
Stéphanie MONNIER
Matthias Napp
Mahavir Prashad
Anton Stuetz
Ranjit Thakur
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to CN2010800305461A priority Critical patent/CN102470134A/en
Priority to JP2012518944A priority patent/JP2012532183A/en
Priority to AU2010270361A priority patent/AU2010270361A1/en
Priority to MX2012000391A priority patent/MX2012000391A/en
Application filed by Novartis Ag filed Critical Novartis Ag
Priority to SG2011095205A priority patent/SG176955A1/en
Priority to EA201200095A priority patent/EA201200095A1/en
Priority to BR112012000383A priority patent/BR112012000383A2/en
Priority to MA34518A priority patent/MA33417B1/en
Priority to CA2767440A priority patent/CA2767440A1/en
Priority to EP10734715A priority patent/EP2451458A2/en
Publication of WO2011003858A2 publication Critical patent/WO2011003858A2/en
Publication of WO2011003858A3 publication Critical patent/WO2011003858A3/en
Priority to TNP2011000653A priority patent/TN2011000653A1/en
Priority to IL217329A priority patent/IL217329A0/en
Priority to ZA2012/00079A priority patent/ZA201200079B/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom

Abstract

The present invention relates to pharmaceutical compositions of 6-(6-hydroxymethyl- pyrimidin-4-yloxy)-naphthalene-1-carboxyfic acid (3-trifluoromethyl-phenyl)-amide, to the use of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthatene-1-carboxylic acid (3-trifluoromethyI- phenyl)-amide and compositions of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-naphthalene-1- carboxylic acid (3-trifluoromethyi-phenyi)-amide in therapeutic applications, especially indications with a dysregulation/overexpression of VEFG, (neo)-vascularisation and VEGF driven angiogenesis and to methods for manufacturing such compositions, the invention further relates to specific forms of 6-(6-hydroxymethyl-pyrimidin-4-yloxy)-πaphthalene-1- carboxyiic acid (3-trifluαromethyl-phenyl)-amide and to the manufacturing and use of such forms. The present invention also relates to a new process to produce 6-{6-hydroxymethyl- pyrimidin-4-yloxy)-naphthalene-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide.
PCT/EP2010/059553 2009-07-06 2010-07-05 Pharmaceutical compositions and solid forms WO2011003858A2 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
EA201200095A EA201200095A1 (en) 2009-07-06 2010-07-05 PHARMACEUTICAL COMPOSITIONS AND SOLID FORMS
AU2010270361A AU2010270361A1 (en) 2009-07-06 2010-07-05 Pharmaceutical compositions and solid forms
MX2012000391A MX2012000391A (en) 2009-07-06 2010-07-05 Pharmaceutical compositions and solid forms.
MA34518A MA33417B1 (en) 2009-07-06 2010-07-05 PHARMACEUTICAL COMPOSITIONS AND SOLID FORMS
SG2011095205A SG176955A1 (en) 2009-07-06 2010-07-05 Pharmaceutical compositions and solid forms
JP2012518944A JP2012532183A (en) 2009-07-06 2010-07-05 Pharmaceutical compositions and solid forms
BR112012000383A BR112012000383A2 (en) 2009-07-06 2010-07-05 pharmaceutical compositions and solid forms
CN2010800305461A CN102470134A (en) 2009-07-06 2010-07-05 Pharmaceutical compositions and solid forms
CA2767440A CA2767440A1 (en) 2009-07-06 2010-07-05 Pharmaceutical compositions and solid forms
EP10734715A EP2451458A2 (en) 2009-07-06 2010-07-05 Pharmaceutical compositions and solid forms
TNP2011000653A TN2011000653A1 (en) 2009-07-06 2011-12-20 Pharmaceutical compositions and solid forms
IL217329A IL217329A0 (en) 2009-07-06 2012-01-02 Pharmaceutical compositions and solid forms
ZA2012/00079A ZA201200079B (en) 2009-07-06 2012-01-05 Pharmaceutical compositions and solid forms

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22326909P 2009-07-06 2009-07-06
US61/223,269 2009-07-06

Publications (2)

Publication Number Publication Date
WO2011003858A2 WO2011003858A2 (en) 2011-01-13
WO2011003858A3 true WO2011003858A3 (en) 2011-03-03

Family

ID=42686504

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2010/059553 WO2011003858A2 (en) 2009-07-06 2010-07-05 Pharmaceutical compositions and solid forms

Country Status (20)

Country Link
US (1) US20110112121A1 (en)
EP (1) EP2451458A2 (en)
JP (1) JP2012532183A (en)
KR (1) KR20120041745A (en)
CN (1) CN102470134A (en)
AR (1) AR077549A1 (en)
AU (1) AU2010270361A1 (en)
BR (1) BR112012000383A2 (en)
CA (1) CA2767440A1 (en)
CO (1) CO6480987A2 (en)
EA (1) EA201200095A1 (en)
EC (1) ECSP12011578A (en)
IL (1) IL217329A0 (en)
MA (1) MA33417B1 (en)
MX (1) MX2012000391A (en)
SG (1) SG176955A1 (en)
TN (1) TN2011000653A1 (en)
TW (1) TW201113258A (en)
WO (1) WO2011003858A2 (en)
ZA (1) ZA201200079B (en)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2008290567B2 (en) 2007-08-17 2011-05-12 Novartis Ag Cyclic depsipeptides
AR086168A1 (en) 2011-04-20 2013-11-27 Novartis Ag PROCESSES FOR THE ELABORATION OF MACROCICLICAL AND INTERMEDIARY DEPSIPEPTIDES
US8680054B2 (en) * 2011-04-20 2014-03-25 Novartis Ag Suspension type topical formulations comprising cyclic depsipeptide
US8987413B2 (en) 2012-10-09 2015-03-24 Novartis Ag Aldehyde acetal based processes for the manufacture of macrocyclic depsipeptides and new intermediates
US9067978B2 (en) 2012-10-09 2015-06-30 Novartis Ag Solution phase processes for the manufacture of macrocyclic depsipeptides and new intermediates
CN104860885B (en) * 2014-02-24 2017-11-17 中国科学院上海药物研究所 Naphthoyl aminated compounds, preparation method and use
SE1751461A1 (en) * 2017-11-28 2019-05-29 Ascilion Ab Method of detecting an exogenous agent in interstitial fluid
WO2019126270A1 (en) * 2017-12-20 2019-06-27 Sienna Biopharmaceuticals, Inc. Formulations for dermal delivery of polymer conjugates of indolocarbazole compounds with reduced exposure

Citations (7)

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WO2002060489A1 (en) * 2001-01-31 2002-08-08 Regeneron Pharmaceuticals, Inc. Method of using a variant of vegf receptor to treat psoriasis and to enhance wound healing
WO2005070891A2 (en) * 2004-01-23 2005-08-04 Amgen Inc Compounds and methods of use
WO2006059234A2 (en) * 2004-09-15 2006-06-08 Novartis Ag Bicyclic amides as kinase inhibitors
WO2007031265A2 (en) * 2005-09-13 2007-03-22 Novartis Ag Combinations comprising a vegf receptor inhibitor and a penetration enhancer
US20070142368A1 (en) * 2005-09-30 2007-06-21 Xiao-Yi Xiao Substituted pyrazole compounds
WO2008009487A1 (en) * 2006-03-10 2008-01-24 Novartis Ag Heterobicyclic carboxamides as inhibitors for kinases
WO2008031835A2 (en) * 2006-09-13 2008-03-20 Novartis Ag Method of treating autoimmune diseases using vegf-pathway inhibitors

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US6355657B1 (en) * 1998-12-30 2002-03-12 Atrix Laboratories, Inc. System for percutaneous delivery of opioid analgesics
AU9458401A (en) * 2000-09-20 2002-04-02 Ortho Mcneil Pharm Inc Pyrazine derivatives as modulators of tyrosine kinases
ES2318649T3 (en) * 2000-10-20 2009-05-01 EISAI R&D MANAGEMENT CO., LTD. PROCEDURE FOR PREPARATION OF DERIVATIVES OF 4-FENOXI QUINOLINAS.
MXPA04007832A (en) * 2002-02-11 2005-09-08 Bayer Pharmaceuticals Corp Aryl ureas with angiogenesis inhibiting activity.
WO2004103159A2 (en) * 2003-05-14 2004-12-02 The Board Of Trustees Of The Leland Stanford Junior University Methods for modulating endometrium
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WO2005070891A2 (en) * 2004-01-23 2005-08-04 Amgen Inc Compounds and methods of use
WO2006059234A2 (en) * 2004-09-15 2006-06-08 Novartis Ag Bicyclic amides as kinase inhibitors
WO2007031265A2 (en) * 2005-09-13 2007-03-22 Novartis Ag Combinations comprising a vegf receptor inhibitor and a penetration enhancer
US20070142368A1 (en) * 2005-09-30 2007-06-21 Xiao-Yi Xiao Substituted pyrazole compounds
WO2008009487A1 (en) * 2006-03-10 2008-01-24 Novartis Ag Heterobicyclic carboxamides as inhibitors for kinases
WO2008031835A2 (en) * 2006-09-13 2008-03-20 Novartis Ag Method of treating autoimmune diseases using vegf-pathway inhibitors

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CHAKRABORTI A K ET AL: "Counterattack mode differential acetylative deprotection of phenylmethyl ethers: Applications to solid phase organic reactions", JOURNAL OF ORGANIC CHEMISTRY 20090206 AMERICAN CHEMICAL SOCIETY USA LNKD- DOI:10.1021/JO801659G, vol. 74, no. 3, 6 February 2009 (2009-02-06), pages 1367 - 1370, XP002615137, ISSN: 0022-3263 *
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Also Published As

Publication number Publication date
ZA201200079B (en) 2012-09-26
MA33417B1 (en) 2012-07-03
CN102470134A (en) 2012-05-23
CO6480987A2 (en) 2012-07-16
BR112012000383A2 (en) 2016-03-29
SG176955A1 (en) 2012-01-30
AU2010270361A1 (en) 2012-01-19
JP2012532183A (en) 2012-12-13
TN2011000653A1 (en) 2013-05-24
WO2011003858A2 (en) 2011-01-13
EP2451458A2 (en) 2012-05-16
CA2767440A1 (en) 2011-01-13
AR077549A1 (en) 2011-09-07
IL217329A0 (en) 2012-02-29
MX2012000391A (en) 2012-02-28
EA201200095A1 (en) 2012-08-30
ECSP12011578A (en) 2012-02-29
US20110112121A1 (en) 2011-05-12
TW201113258A (en) 2011-04-16
KR20120041745A (en) 2012-05-02

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